[CAS NO. 2226534-49-0] Y06137
PRODUCTS SPECIFICATIONS [2226534-49-0]
DESCRIPTION [2226534-49-0]
Overview
| MDL | MFCD31813648 |
|---|---|
| Molecular Weight | 444.57 |
| Molecular Formula | C27H32N4O2 |
| SMILES | CC1=NOC(C1=C2)=CC=C2C3=NC(C=C4)=C(N3CC5CCCCC5)C=C4N6CCOC[C@@H]6C |
Summary
IC50 & Target
|
BRD4(1) 81 nM (Kd) |
In Vitro
Y06137 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC 50 : 0.29-2.6 μΜ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06137 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | AR-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP |
| Concentration: | 0.001-100 μM |
| Incubation Time: | 96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaP |
| Result: | Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC 50 s of 0.47, 0.84, 0.70, 0.29 μM, respectively. |
Western Blot Analysis [1]
| Cell Line: | AR-positive prostate cancer cell lines 22Rv1 |
| Concentration: | 1, 2, 4, 8, and 16 μM |
| Incubation Time: | 48 hours |
| Result: | Resulted in significant down-regulation of both AR-fl and AR variants levels. |
In Vivo
Y06137 (50 mg/kg, i.p. injection, 5 times per week, 25 days) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06137 is well tolerated in the treated mice, based on the weight of the animal body and their general behavior [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Four-week-old male mice (strain: C.B-17/IcrHsd- Prkdc scid for C4-2B) with C4-2B mouse xenograft model [1] |
| Dosage: | 50 mg/kg, 100 μL |
| Administration: | Intraperitoneal (i.p.) injection, 5 times per week, 25 days |
| Result: | Exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 51%. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 140.59 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2494 mL | 11.2468 mL | 22.4936 mL |
| 5 mM | 0.4499 mL | 2.2494 mL | 4.4987 mL |
| 10 mM | 0.2249 mL | 1.1247 mL | 2.2494 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution
